COMPOUNDS AND THEIR THERAPEUTIC USE RELATED TO THE PHOSPHORYLATING ACTIVITY OF THE ENZYME GSK-3

摘要

Compounds of formula (I): wherein: X represents CH=CH-, -CH=CR-, -CR=CR-, -CO-, -O-, -NH-, -NR-, -S-, -SO-, -SO2-, -CH=N-, -CR=N-, -CH=N(O)-, -CR=N(O)- or any other atom or groug of atoms capable of forming a S- or 6- membered heterocyclic ring; Y1, Y2 and Y3 independently represent hydrogen or halogen; R1, R2 and R3 are independently represent hydrogen, halogen, hydrocarbyl (-R), hydroxyl (-OH), hydrocarbyloxy (-O-R), mercapto (-SH), hydrocarbylthio (-S-R), hydrocarbylsulfinyl (-SO-R), hydrocarbylsulfonyl (-SO2-R), nitro (-NO2), amino (-NH2), hydrocarbylamino (-NHR), bis(hydrocarbyl)amino (-NR2), hydrocarbylcarbonylamino (-NH-CO-R), cyano (-CN), carbamoyl (-CONH2), hydrocarbylcarbamoyl (-CONHR), bis(hydrocarbyl)carbamoyl (-CONR2), carboxyl (-CO2H), hydrocarbyloxycarbonyl (-CO2R), formyl (-CHO), hydrocarbylcarbonyl (-COR), hydrocarbylcarbonyloxy (-OCOR), optionally substituted heteroaryl or optionally substituted hetereocyclic; and the hydrocarbyl group R is a straight or branched chain hydrocarbyl group selected from alkyl, alkenyl, alkynyl, aryl, aralkyl, aralkenyl and aralkynyl, which may optionally be subtituted by one or more substituents, selected from those defined above in relation to R1, R2, and R3] ; are of use in the manufacture of a medicament for the treatment including prophylaxis of disease mediated by the activation of GSK-3.